What is the clinical significance of Nystatin (antifungal medication) to human health?

From the Guidelines

Nystatin is a valuable antifungal medication for treating localized Candida infections, particularly in immunocompromised patients, infants, and pregnant women, due to its minimal systemic absorption and low risk of fungal resistance 1.

Clinical Significance of Nystatin

Nystatin works by binding to sterols in the fungal cell membrane, creating pores that lead to cell death. It is most commonly prescribed for:

• Oral thrush (as an oral suspension, 400,000-600,000 units 4 times daily for 7-14 days)
• Vaginal yeast infections (as suppositories or cream)
• Cutaneous candidiasis (as cream or ointment applied 2-3 times daily until 48 hours after symptoms resolve)

Key Benefits of Nystatin

• Minimal systemic absorption, making it safer than systemic antifungals for treating localized infections
• Low risk of fungal resistance, making it a valuable option for long-term treatment
• Mild side effects, including nausea, vomiting, or gastrointestinal upset with oral formulations, or local irritation with topical applications

Recommendations for Use

• For mild disease, nystatin suspension (100,000 U/mL) 4–6 mL 4 times daily, or 1–2 nystatin pastilles (200,000 U each) 4 times daily, for 7–14 days is recommended (strong recommendation; moderate-quality evidence) 1
• For moderate to severe disease, oral fluconazole, 100–200 mg daily, for 7–14 days is recommended (strong recommendation; high-quality evidence) 1

Important Considerations

• Nystatin should be used with caution in patients with known hypersensitivity to the medication
• Patients should be advised to swish the oral suspension around the mouth before swallowing or apply it directly to affected areas for optimal effectiveness
• Nystatin is not recommended for systemic infections, as it is not absorbed well and may not reach effective concentrations in the bloodstream 1

From the FDA Drug Label

CLINICAL PHARMACOLOGY Pharmacokinetics Gastrointestinal absorption of nystatin is insignificant. Most orally administered nystatin is passed unchanged in the stool. In patients with renal insufficiency receiving oral therapy with conventional dosage forms, significant plasma concentrations of nystatin may occasionally occur Microbiology Nystatin is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeast-like fungi. Candida albicans demonstrates no significant resistance to nystatin in vitro on repeated subculture in increasing levels of nystatin; other Candida species become quite resistant. Generally, resistance does not develop in vivo Nystatin acts by binding to sterols in the cell membrane of susceptible Candida species with a resultant change in membrane permeability allowing leakage of intracellular components. Nystatin exhibits no appreciable activity against bacteria, protozoa, or viruses.

The clinical significance of Nystatin to human health is that it is effective against fungal infections, specifically Candida species. It works by binding to sterols in the cell membrane, causing a change in membrane permeability and allowing leakage of intracellular components, ultimately leading to the death of fungal cells. This makes Nystatin a valuable treatment option for fungal infections [ 2 ].

• Key benefits: fungistatic and fungicidal properties, effective against a wide variety of yeasts and yeast-like fungi.
• Important consideration: Nystatin has no appreciable activity against bacteria, protozoa, or viruses.

From the Research

Clinical Significance of Nystatin

The clinical significance of Nystatin, an antifungal medication, is evident in its effectiveness against various Candida species, which are common causes of oral candidiasis. Key points regarding its clinical significance include:

• Nystatin is a common antifungal agent used topically for the treatment of oral candidiasis, with studies showing its efficacy in clinical and mycological cure rates 3, 4.
• The medication has been found to be equally effective as photodynamic therapy for the clinical remission of denture stomatitis and significant reduction of CFU/mL of Candida species from dentures and palatal surfaces of patients 3.
• Nystatin pastille has been shown to be significantly superior to placebo in treating denture stomatitis, although nystatin suspension was not superior to fluconazole in treating oral candidiasis in infants, children, or HIV/AIDS patients 4.
• The use of nystatin pastilles alone or in combination with nystatin suspensions has been found to be more effective than using nystatin suspensions alone, with prolonged treatment duration up to 4 weeks increasing the efficacy of nystatin 4.
• Nystatin, along with miconazole and fluconazole, is considered very effective for treating oral candidiasis, with systemic alternatives available for recalcitrant infections 5.
• The post-antifungal effect (PAFE) of nystatin on Candida species of oral origin has been studied, with variations in PAFE amongst non-albicans species potentially having clinical implications for nystatin regimens 6.
• Recent developments include the characterization and antifungal evaluation of nystatin:β-cyclodextrin inclusion complexes, which have shown improved drug solubility, dissolution, and sustained delivery, and effectively inhibited C. albicans biofilm growth 7.

Mechanism of Action and Efficacy

The mechanism of action of nystatin involves binding to the fungal cell membrane, causing changes in membrane permeability and ultimately leading to cell death. Its efficacy against various Candida species has been demonstrated in several studies, including:

• A systematic review and meta-analysis of clinical trials, which found nystatin to be effective in treating oral candidiasis, particularly when used as a pastille 4.
• A study on the therapeutic tools for oral candidiasis, which highlighted nystatin as one of the most commonly used topical antifungal drugs, along with miconazole 5.
• An investigation on the PAFE of nystatin on oral isolates of Candida, which found significant variations in PAFE amongst non-albicans species 6.
• A characterization and antifungal evaluation of nystatin:β-cyclodextrin inclusion complexes, which showed improved drug delivery and efficacy against C. albicans biofilm growth 7.

Treatment Protocols and Safety

Treatment protocols for nystatin vary depending on the formulation, dosage, and duration of treatment. Key points regarding treatment protocols and safety include:

• Nystatin pastilles are often used for the treatment of denture stomatitis, with a dose of 400,000 IU resulting in a significantly higher mycological cure rate than a dose of 200,000 IU 4.
• Treatment with nystatin pastilles for 4 weeks has been found to have better clinical efficacy than treatment for 2 weeks 4.
• The safety of nystatin has been assessed, with poor taste and gastrointestinal adverse reactions being the most common adverse effects 4.
• The use of nystatin:β-cyclodextrin inclusion complexes has been found to improve drug solubility, dissolution, and sustained delivery, potentially reducing the risk of adverse effects 7.